TRP Channel

Transient receptor potential (TRP) channels are cellular sensors for a wide spectrum of physical and chemical stimuli. They are involved in the formation of sight, hearing, touch, smell, taste, temperature, and pain sensation. TRP channels also play fundamental roles in cell signaling and allow the host cell to respond to benign or harmful environmental changes.

GsMTx4
M 084 hydrochloride
RN 1747
1024448-59-6
CIM 0216
1031496-06-6
1041478-78-7
AMG8562
1041478-78-7
OLDA
105955-11-1
MK6-83
1062271-24-2
EIPA
1154-25-2
TC-I 2000
1159996-20-9
Pyr3
1160514-60-2
B0084-359603
A 967079
1170613-55-4
ASP 7663
1190217-35-6
TRPV antagonist 1
1192871-27-4
TC-I 2014
1221349-53-6
A-1165442
1221443-94-2

Background


An overview of TRP Channel

Transient receptor potential (TRP) is a kind of important non-selective cation channel super family located on the cell membrane, and the ions that can pass are mainly sodium ions, calcium ions and magnesium ions. It can be divided into six subfamilies, including TRPC, TRPV, TRPM, TRPA, TRPP and TRPML. And the TRPC has a hydrophobic 6-transmembrane structure and a nitrogen (N) end and a carbon (C) end in the cell. They are involved in the formation of sight, hearing, touch, smell, taste, temperature, and pain sensation.

The TRPC family includes seven subtypes, including TRPC1~7, and they can be divided into four subgroups, including TRPC1, TRPC2, TRPC4/5, and TRPC3/6/7, among which the TRPC2 is only expressed in rats and mice, while it is a pseudo gene in human and the rest are expressed in the human central nervous system, and the TRPC3 is mainly expressed in the membrane structure of the oligodendroglia cell.

Inhibition of TRP Channel

Pico145 is an efficient TRPC1/TRPC4/TRPC5 inhibitor, which inhibits (-)-englerin A-activated TRPC4/TRPC5 in cells, and its IC 50 is 0.349 and 1.3 nM. And it has no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2 and TRPM8.

TRP Channel and diseases

Some studies have found that activation or overexpression of TRPC in human neuroblastoma cell SH-SYSY can reduce the apoptosis induced by MPP. In addition, TRPCI-mediated calcium ions in the intestinal endothelial cells can inhibit the activation of NF-κB and induce cell apoptosis. It was also found that in myocardial, the overexpression of TRPC3 can induce apoptosis of the myocardial cells. Thus, it is shown that intracellular calcium concentration is closely related to cell damage, and TRPC can lead to the change of intracellular calcium concentration. And the cell apoptosis mechanism can be initiated if the concentration of calcium ions increases.